Lidocaine (lidocaine)

Topical Local Anesthetics Topical Cream (Gram); Topical Kit

Advertisement

Last reviewed · Source: First Databank (FDB) drug data

Overview

Lidocaine, a nonselective voltage-gated sodium channel inhibitor, is an amide-type local anesthetic.

Lidocaine is an amide-type local anesthetic that blocks sodium ion channels required for the initiation and conduction of neuronal impulses. The analgesic effects of lidocaine are thought to result from these effects. Penetration of lidocaine into intact skin is sufficient to produce an analgesic effect; however, the amount is insufficient to produce a complete sensory block.

Ztlido(R) (lidocaine topical system) 1.8% is a single-layer, drug-in-adhesive, topical deliverysystem comprised of an adhesive material containing 36 mg lidocaine, which is applied toa pliable nonwoven cloth backing and covered with a polyethylene terephthalate (PET) filmrelease liner. Lidoderm(R) transdermal patch is composed of an adhesive material containing 5%lidocaine, which is applied to a nonwoven polyester felt backing and covered with aPET film release liner. The release liner is removed prior toapplication of both the Ztlido(R) and Lidoderm(R) patches.

The amount of lidocaine that is systemically absorbed from a lidocaine patch is directly related toboth the duration of application and the surface area over which it is applied. There is minimal systemic absorption (approximately 3%) when the 5% patches are used topically as recommended and maximum blood concentrations are about 1/10 of the therapeutic concentration required to treat cardiac arrhythmias. In apharmacokinetic study evaluating lidocaine 5% patches, 3 patches (total of 2100 mg) were applied over an area of 420 cm2of intact skin on the backs of normal volunteers for 12 hours.

The total dose absorbed was approximately 64 mg and time to peak plasma concentration was 11 hours. Mean lidocaine blood concentrations after 3 consecutive days of daily use (3 patches applied at the same time for 12 hours once daily for 3 days) remained the same. In a pharmacokinetic study evaluating the 1.8% patches, 3 patches (total dose of 108 mg) were applied over an area of 420 cm2of intact skin on the backs of normal volunteers for 12 hours.

Time to peak plasma concentration was approximately 14 hours. Mean lidocaine blood concentrations after 3 consecutive days of daily use (3 patches applied at the same time for 12 hours once daily for 3 days) remained the same.

Lidocaine is approximately 70% bound to plasma proteins (primarily alpha-1-acid glycoprotein) at concentrations achieved from topical application; at higher concentrations, plasma protein binding is concentration dependent. Lidocaine crosses the placental and blood brain barriers, presumably by diffusion. It is not known if lidocaine is metabolized in the skin.

However, lidocaine is extensively metabolized in the liver to several pharmacologically active metabolites and is excreted by the kidneys (less than 10% as unchanged drug).

Lidocaine 1.8% patches (Ztlido(R)) are bioequivalent to lidocaine 5% patches (Lidoderm(R) and generics).

Lidocaine is used topically for the treatment of pain. Various topical lidocaine products are commercially available. Lidocaine 1.8% and 5% topical systems (i.e., patches) are FDA-labeled for the treatment of pain associated with postherpetic neuralgia (PHN).

Lidocaine is also available in various over-the-counter (OTC) topical preparations for the temporary treatment of pain.

Generic name: lidocaine
Drug class: Topical Local Anesthetics
Therapeutic class: Dermatological

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

Today’s intelligence on Lidocaine

Intelligence content is not available yet.

Indications

The following indications are listed for Lidocaine:

  • Hemorrhoids
  • Proctitis
  • Pruritus Ani
  • Rectal Pain

Also known as: Proctalgia, Rectitis.

Dosing

No dosing information is available for this tab.

Drug interactions

There is no enhanced messaging for this drug.

Contraindications

*Known history of sensitivity to local anesthetic of the amide type, or to any other component of the product.

Adverse reactions

Common adverse effects of lidocaine 1.8 and 5% patches include mild and transient application site reactions (e.g., blisters, bruising, burning sensation, depigmentation,dermatitis, discoloration, edema, erythema, exfoliation, irritation, papules, petechia,pruritus, vesicles).

Systemic adverse reactions following topical use of lidoderm patch are unlikely due to minimal drug absorption.

Precautions

No enhanced messaging available.

ICD codes

CodeTypeDescription
Hemorrhoids
K64.0ICD10CMFirst degree hemorrhoids
K64.8ICD10CMOther hemorrhoids
K64.9ICD10CMUnspecified hemorrhoids
O22.4ICD10CMHemorrhoids in pregnancy
O22.40ICD10CMHemorrhoids in pregnancy, unspecified trimester
O22.41ICD10CMHemorrhoids in pregnancy, first trimester
O22.42ICD10CMHemorrhoids in pregnancy, second trimester
O22.43ICD10CMHemorrhoids in pregnancy, third trimester
O87.2ICD10CMHemorrhoids in the puerperium
Proctitis
K62.7ICD10CMRadiation proctitis
K62.89ICD10CMOther specified diseases of anus and rectum
Pruritus ani
L29.0ICD10CMPruritus ani
L29.3ICD10CMAnogenital pruritus, unspecified
Pruritus of skin
L29.8ICD10CMOther pruritus
L29.81ICD10CMCholestatic pruritus
L29.89ICD10CMOther pruritus
L29.9ICD10CMPruritus, unspecified
Rectal pain
K62.89ICD10CMOther specified diseases of anus and rectum
Skin irritation
L24ICD10CMIrritant contact dermatitis
L24.0ICD10CMIrritant contact dermatitis due to detergents
L24.1ICD10CMIrritant contact dermatitis due to oils and greases
L24.2ICD10CMIrritant contact dermatitis due to solvents
L24.3ICD10CMIrritant contact dermatitis due to cosmetics
L24.4ICD10CMIrritant contact dermatitis due to drugs in contact with skin
L24.5ICD10CMIrritant contact dermatitis due to other chemical products
L24.6ICD10CMIrritant contact dermatitis due to food in contact with skin
L24.7ICD10CMIrritant contact dermatitis due to plants, except food
L24.8ICD10CMIrritant contact dermatitis due to other agents
L24.81ICD10CMIrritant contact dermatitis due to metals
L24.89ICD10CMIrritant contact dermatitis due to other agents
L24.9ICD10CMIrritant contact dermatitis, unspecified cause
L24.AICD10CMIrritant contact dermatitis due to friction or contact with body fluids
L24.A0ICD10CMIrritant contact dermatitis due to friction or contact with body fluids, unspecified
L24.A1ICD10CMIrritant contact dermatitis due to saliva
L24.A2ICD10CMIrritant contact dermatitis due to fecal, urinary or dual incontinence
L24.A9ICD10CMIrritant contact dermatitis due friction or contact with other specified body fluids
L24.BICD10CMIrritant contact dermatitis related to stoma or fistula
L24.B0ICD10CMIrritant contact dermatitis related to unspecified stoma or fistula
L24.B1ICD10CMIrritant contact dermatitis related to digestive stoma or fistula
L24.B2ICD10CMIrritant contact dermatitis related to respiratory stoma or fistula
L24.B3ICD10CMIrritant contact dermatitis related to fecal or urinary stoma or fistula
L25ICD10CMUnspecified contact dermatitis
L25.0ICD10CMUnspecified contact dermatitis due to cosmetics
L25.1ICD10CMUnspecified contact dermatitis due to drugs in contact with skin
L25.2ICD10CMUnspecified contact dermatitis due to dyes
L25.3ICD10CMUnspecified contact dermatitis due to other chemical products
L25.4ICD10CMUnspecified contact dermatitis due to food in contact with skin
L25.5ICD10CMUnspecified contact dermatitis due to plants, except food
L25.8ICD10CMUnspecified contact dermatitis due to other agents
L25.9ICD10CMUnspecified contact dermatitis, unspecified cause
L30.9ICD10CMDermatitis, unspecified
R21ICD10CMRash and other nonspecific skin eruption

ICD code information from First Databank (FDB).

Formulary status

Search health-plan coverage for this drug by ZIP code.

Enter a ZIP code to view available health plans.

Last reviewed · Source: First Databank (FDB) drug data